Abstract

In this study, combination-principle was reported to improve the hepatoprotective activity of andrographolide. Ten andrographolide derivatives were synthesized and evaluated for in vivo hepatoprotective activity in CCl4-induced liver injury mice. The pharmacological results revealed that 6 derivatives exhibited significant hepatoprotective activity. The most promising compound 6b significantly improved liver enzymes (ALT and AST) activity as compared with andrographolide, with high potency to be a new lead.